Lenvatinib (E7080)

- Overview
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    Background
    
    Lenvatinib (E7080) is an inhibitor of multiple RTK with IC50 values of 22 nM, 4 nM, 5.2 nM, 39 nM and 35 nM on VEGFR-1, VEGFR-2, VEGFR-3, PDGFRβ and RET, respectively [1].
    Lenvatinib is presently under investigation both as monotherapy and in combination with cytotoxic agents for multiple types of solid tumor, including thyroid carcinoma and hepatocellular carcinoma (in Phase III trials), and melanoma, renal carcinoma, non-small cell lung carcinoma, glioblastoma multiforme, and ovarian and endometrial carcinoma (Phase I and II trials) [1].
    When used as an inhibitor of RET kinase, Lenvatinib cause growth inhibition in TPC-1 cells and LC-2/ad cells. The GI50 values are 27 nM and 48 nM. It is also reported that Lenvatinib can inhibit RET (rearranged during transfection) gene fusion kinases, and inhibit oncogenic signaling of RET gene fusions. Lenvatinib has been demonstrated to exert antitumor activities in RET gene fusion-driven tumor models [2].
    
    [1] Neda Stjepanovic, Jaume Capdevila. Multikinase inhibitors in the treatment of thyroid cancer: specific role of lenvatinib. Biologics: Targets and Therapy. 2014 (8): 129-139.
    [2] Kiyoshi Okamoto, Kotaro Kodama, Kazuma Takase, Naoko Hata Sugi, Yuji Yamamoto, Masao Iwata, Akihiko Tsuruoka. Antitumor activities of the targeted multi-tyrosine kinase inhibitor lenvatinib (E7080) against RET gene fusion-driven tumor models. Cancer Letters. 2013 July (340): 97-103.
- Properties
  - Alternative Name
    
    4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide
    
    CAS Number
    
    417716-92-8
    
    Molecular Formula
    
    C21H19ClN4O4
    
    Molecular Weight
    
    426.85
    
    Purity
    
    99.87%
    
    Solubility
    
    ≥21.35 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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Lenvatinib (E7080)

Background

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